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Titolo:
Application of pressure-controlled colon delivery capsule to oral administration of glycyrrhizin in dogs
Autore:
Shibata, N; Ohno, T; Shimokawa, T; Hu, ZP; Yoshikawa, Y; Koga, K; Murakami, M; Takada, K;
Indirizzi:
Kyoto Pharmaceut Univ, Dept Pharmacokinet, Yamashima Ku, Kyoto 6078414, Japan Kyoto Pharmaceut Univ Kyoto Japan 6078414 shima Ku, Kyoto 6078414, Japan Hokuriku Univ, Fac Pharmaceut Sci, Dept Pharmaceut, Kanazawa, Ishikawa, Japan Hokuriku Univ Kanazawa Ishikawa Japan rmaceut, Kanazawa, Ishikawa, Japan
Titolo Testata:
JOURNAL OF PHARMACY AND PHARMACOLOGY
fascicolo: 4, volume: 53, anno: 2001,
pagine: 441 - 447
SICI:
0022-3573(200104)53:4<441:AOPCDC>2.0.ZU;2-U
Fonte:
ISI
Lingua:
ENG
Soggetto:
GASTROINTESTINAL ABSORPTION; DOSAGE FORMS; BEAGLE DOGS; ACID; DRUG; BIOAVAILABILITY; RATS; CHROMATOGRAPHY; DISSOLUTION; RELEASE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Takada, K Kyoto Pharmaceut Univ, Dept Pharmacokinet, Yamashima Ku, Kyoto 6078414, Japan Kyoto Pharmaceut Univ Kyoto Japan 6078414 Kyoto 6078414, Japan
Citazione:
N. Shibata et al., "Application of pressure-controlled colon delivery capsule to oral administration of glycyrrhizin in dogs", J PHARM PHA, 53(4), 2001, pp. 441-447

Abstract

A colon delivery system has been used to improve the bioavailability of glycyrrhizin, a glycoside of glycyrrhetic acid. The bioavailability of glycyrrhizin is low when administered in conventional oral galenic dosage forms because glycyrrhizin is enzymatically hydrolysed both in the stomach and in the intestine, it was reasoned that if large amounts of glycyrrhizin were directly delivered to the colon, enzymatic activity should be reduced due tosaturation so that intact glycyrrhizin could be absorbed into the systemiccirculation. Based on this assumption, pressure-controlled colon delivery capsules (PCDCs) were used as a colon delivery system. Eight types of glycyrrhizin solution were prepared and were introduced into PCDCs. After oral administration of the test PCDCs to beagle dogs, blood samples were obtainedover 24 h and plasma glycyrrhizin concentrations were measured by an HPLC method. With PCDCs containing aqueous glycyrrhizin and propylene glycol solutions, plasma glycyrrhizin levels were extremely low and the bioavailabilities of glycyrrhizin were 0.6 % and 0.4 %, respectively. When Labrasol was added to both types of glycyrrhizin solution, the bioavailability was improved to 4.6 % for aqueous solution and 3.8 % for propylene glycol solution. When a surfactant, Polysorbate 80, was added in combination with Labrasol, synergistic effects were not obtained. Furthermore, dose-dependent effects of Polysorbate 80 were not obtained. Labrasol, which is a component of self-emulsifying drug delivery systems (SEDDS), has been shown to strongly improve the bioavailability of glycyrrhizin from the colon.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 10/07/20 alle ore 07:27:53